2-{[N-(2-amino-3-(heteroaryl or aryl) propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives
0 Assignments
0 Petitions
Accused Products
Abstract
The present invention relates to compounds of formula I
-
Citations
22 Claims
-
1-20. -20. (canceled)
-
21. A pharmaceutical composition for the treatment of a proliferative disease in warm-blooded animals, including humans, comprising, in a dose effective against said disease, a compound according to formula I
wherein R1 is unsubstituted or substituted aryl; - arylalkylcarbonyl, wherein the aryl moiety is unsubstituted or substituted;
unsubstituted or substituted heterocyclyl;
or heterocyclylalkylcarbonyl, wherein the heterocyclyl moiety is unsubstituted or substituted;
R2 is unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl;
R3 is hydrogen, unsubstituted or substituted aryl or alkyl which is unsubstituted or substituted by unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl comprising at least one nitrogen atom;
R4 is a moiety of the formula IA, wherein A1 and A2 are hydroxy or substituted hydroxy, or together with the binding boron atom and the two binding oxygen atoms form a ring of the formula IA*, wherein W is alkylene, substituted alkylene, unsubstituted or substituted cycloalkylene, unsubstituted or substituted bicycloalkylene or unsubstituted or substituted tricycloalkylene;
and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, or unsubstituted or substituted cycloalkyl;
or a pharmaceutically acceptable salt of such a compound, together with a pharmaceutically acceptable carrier, wherein the proliferative disease is selected from psoriasis, restenosis, muscle protein degradation or other diseases connected with intracellular protein degradation or negative nitrogen balance, sepsis, burns, trauma, chronic or systemic infections, neuromotor degenerative disease, muscular dystrophia, acidosis, spinal or nerve injuries, diseases related to antigen presentation on cells; and
diseases related to cell adhesion.
- arylalkylcarbonyl, wherein the aryl moiety is unsubstituted or substituted;
-
22. A method of treating warm-blooded animals, including humans, which comprises administering to such warm-blooded animal suffering from a proliferative disease a dose, effective against said disease, of a compound according to formula I
wherein R1 is unsubstituted or substituted aryl; - arylalkylcarbonyl, wherein the aryl moiety is unsubstituted or substituted;
unsubstituted or substituted heterocyclyl;
or heterocyclylalkylcarbonyl, wherein the heterocyclyl moiety is unsubstituted or substituted;
R2 is unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl;
R3 is hydrogen, unsubstituted or substituted aryl or alkyl which is unsubstituted or substituted by unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl comprising at least one nitrogen atom;
R4 is a moiety of the formula IA, wherein A1 and A2 are hydroxy or substituted hydroxy, or together with the binding boron atom and the two binding oxygen atoms form a ring of the formula IA*, wherein W is alkylene, substituted alkylene, unsubstituted or substituted cycloalkylene, unsubstituted or substituted bicycloalkylene or unsubstituted or substituted tricycloalkylene;
and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, or unsubstituted or substituted cycloalkyl;
or of a pharmaceutically acceptable salt of such a compound, wherein the proliferative disease is selected from psoriasis, restenosis, muscle protein degradation or other diseases connected with intracellular protein degradation or negative nitrogen balance, sepsis, burns, trauma, chronic or systemic infections, neuromotor degenerative disease, muscular dystrophia, acidosis, spinal or nerve injuries, diseases related to antigen presentation on cells; and
diseases related to cell adhesion.
- arylalkylcarbonyl, wherein the aryl moiety is unsubstituted or substituted;
Specification